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Literature summary for 3.4.21.B39 extracted from

  • Debela, M.; Goettig, P.; Magdolen, V.; Huber, R.; Schechter, N.M.; Bode, W.
    Structural basis of the zinc inhibition of human tissue kallikrein 5 (2007), J. Mol. Biol., 373, 1017-1031.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in a baculovirus-insect cell system Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
crystallized in complex with leupeptin, sitting drop vapour diffusion method with 0.2 M ammonium sulfate, 0.1 M Mes (pH 5.6) and 30% (w/v) PEG monomethyl ether 500 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
leupeptin
-
Homo sapiens
Zn2+ non-competitive inhibition, the enzyme activity is restored by addition of EDTA showing reversibility Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
30000
-
SDS-PAGE Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y337
-
-

Purification (Commentary)

Purification (Comment) Organism
heparin-Sepharose column chromatography and benzamidine-Sepharose column chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
skin
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Cbz-L-Pro-Phe-Arg-p-nitroanilide + H2O
-
Homo sapiens Cbz-L-Pro-Phe-Arg + 4-nitroaniline
-
?
L-Pro-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens L-Pro-Phe-Arg + 7-amino-4-methylcoumarin
-
?
tosyl-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens tosyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
K5
-
Homo sapiens
kallikrein-like protein 2
-
Homo sapiens
KLK-L2
-
Homo sapiens
tissue kallikrein 5
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0017
-
leupeptin at 25°C in 0.2 M NaCl, 0.1 M Tris-HCl (pH 8.0), and 9% (w/v) Me2SO Homo sapiens
0.002
-
Zn2+ in 150 mM NaCl, 20 mM HEPES, 0.04 mM imidazole, 0.005% (v/v) Tween 20, at pH 8.0 Homo sapiens
0.008
-
Zn2+ in 150 mM NaCl, 20 mM HEPES, 0.04 mM imidazole, 0.005% (v/v) Tween 20, at pH 7.0 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.009
-
in 150 mM NaCl, 20 mM HEPES, 0.04 mM imidazole, 0.005% (v/v) Tween 20, at pH 7.0 Homo sapiens Zn2+